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Assay Detail

CHEMBL826591

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Functional
Inhibition of (10 uM) forskolin-mediated cAMP production in CHO cells expressing human Adenosine A3 receptor
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Expert

Target

Adenosine receptor A3 (CHEMBL256)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and biological evaluation of novel N6-[4-(substituted)sulfonamidophenylcarbamoyl]adenosine-5'-uronamides as A3 adenosine receptor agonists.
Baraldi PG, Fruttarolo F, Tabrizi MA, Romagnoli R, Preti D, Bovero A, Pineda de Las Infantas MJ, Moorman A, Varani K, Borea PA.
J Med Chem (2004) 47 : 5535 -5540
PubMed 15481989 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 7.48 8.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL431733 NAMODENOSON 3.0 1 8.66
CHEMBL611095 1 7.38
CHEMBL611091 1 7.30
CHEMBL608755 1 7.26
CHEMBL611104 1 7.19
CHEMBL265587 1 7.09

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL431733 NAMODENOSON IC50 = 2.2 nM 8.66
CHEMBL611095 IC50 = 42.0 nM 7.38
CHEMBL611091 IC50 = 50.0 nM 7.30
CHEMBL608755 IC50 = 55.0 nM 7.26
CHEMBL611104 IC50 = 65.0 nM 7.19
CHEMBL265587 IC50 = 81.0 nM 7.09